Synthesis of Cryptophycin Affinity Labels and Tubulin Labeling
Annual summary rept. 1 May 2004-30 Apr 2005
KANSAS UNIV CENTER FOR RESEARCH INC LAWRENCE
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Cryptophycins are a potent, tumor-selective class of tubulin-binding antimitotic anti-cancer agents with excellent activity against MDR cancers. In order to develop these promising compounds into useful chemotherapeutic agents, it is necessary to obtain detailed information about the binding domain of the cryptophycins on tubulin. We plan to map the cryptophycin binding site through photoaffinity labeling studies. Toward this goal we have synthesized and studied the activity of a C16 side chain benzophenone photoaffinity analogues as well as a C10 azido analogues of cryptophycin-24. We have prepared a radioactive photoaffinity analogue and have initiated photolabeling studies. In addition, we are reporting an improved synthetic route to achieve the synthesis of diverse analogues in a more efficient way.
- Medicine and Medical Research